Ibicuruzwa

4- [6- (6-bromo-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido piperazine-1-karubasi ya acide tert-butyl ester nuruvange rushobora gukoreshwa mubushakashatsi bwa farumasi no guteza imbere ibiyobyabwenge.Imiterere igoye hamwe nitsinda ryimikorere bitanga amahirwe atandukanye yo gukora iperereza no gushakisha uburyo bwo kuvura.Ibishoboka bishoboka ko iyi nteruro iri murwego rwa oncology.Kuba hari itsinda rya bromo hamwe na pyrido [2,3-d] pyrimidin moyety yerekana ko ishobora kuba ifite ibikorwa byo kurwanya kanseri.Itsinda rya bromo rizwiho ubushobozi bwo guhagarika imikurire ya selile no gutera apoptose muri selile.Byongeye kandi, pyrido [2,3-d] pyrimidin scafold yajyanye ningaruka zo kurwanya no gukwirakwiza ibibyimba.Rero, uru ruganda rushobora kwigwa cyane kubushobozi bwarwo nk'igitabo gishya cyo kurwanya kanseri.Ikindi kandi, amatsinda ya cyclopentyl na methyl aboneka muri iyo miterere akora lipofilique, ishobora kugira uruhare mu bushobozi bwayo bwo kurenga inzitizi zishingiye ku binyabuzima, nk'amaraso -inzitizi y'ubwonko.Uyu mutungo ufungura amahirwe yo kuwukoresha mugutezimbere imiti yibasira indwara zifata imitsi yo hagati, nk'indwara zifata ubwonko.Uru ruganda rushobora guhindurwa kugirango rwongere ubushobozi bwarwo hamwe nububasha bwo kurwanya intego zihariye ziterwa nizi ndwara. Byongeye kandi, kuba piperazine-1-karubasi ya acide tert-butyl ester moiety yerekana ko uruganda rushobora kugira akamaro nka prodrug.Prodrugs ni ibintu bidakora bishobora guhinduka muburyo bukora mumubiri.Itsinda rya tert-butyl ester rirashobora gukora nkitsinda ririnda, ririnda gukora hakiri kare ibiyobyabwenge mbere yuko bigera aho bifuza.Iyo igeze ku ntego cyangwa ingirabuzimafatizo, itsinda rya ester rishobora gutoborwa mu buryo bwa ferime, rikarekura molekile ikora ibiyobyabwenge.Ikindi kandi, piridine hamwe na pyrimidine yimvange yerekana ubushobozi bwayo nka farumasi yo gukora imiti ihitamo imisemburo yihariye cyangwa iyakira.Ibi birashobora kuva kuri kinase kugeza kuri G protein-ihujwe na reseptor, bitewe nimpinduka zakozwe muburyo bwibanze.Uru ruganda rushobora kuba intangiriro yubushakashatsi bwibikorwa byubaka kandi bikayobora uburyo bwiza bwo guteza imbere inzitizi zikomeye zo guhitamo intego zihariye zo kuvura.Mu ncamake, 4- [6- (6-bromo-8-cyclopentyl-5-methyl-7 -oxo-7,8-dihydro-pyrido [2,3-d] pyrimidin-2-ylamino) -pyridin-3-yl] -piperazine-1-karubasi ya acide tert-butyl ester yerekana ubushobozi mubice bitandukanye byubushakashatsi bwa farumasi.Imiterere yihariye hamwe nitsinda ryimikorere irashobora gushakishwa cyane mubikorwa byo kurwanya kanseri, guteza imbere imiti yo hagati y’imiti, ingamba za prodrug, hamwe na enzyme yatoranijwe cyangwa kubuza reseptor.Gukomeza iperereza no gutezimbere iki kigo bishobora kuganisha ku kuvumbura uburyo bushya bwo kuvura hamwe no kunoza imikorere hamwe nintego yihariye.